Oflo^® (Tablets, Solution) Instructions for Use

ATC Code

J01MA01 (Ofloxacin)

Active Substance

Ofloxacin (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Antibacterial drug of the fluoroquinolone group

Pharmacotherapeutic Group

Antimicrobial agent – fluoroquinolone

Pharmacological Action

A broad-spectrum antimicrobial drug from the fluoroquinolone group, it acts on the bacterial enzyme DNA gyrase, which provides supercoiling and thus the stability of bacterial DNA (destabilization of DNA chains leads to their death). It has a bactericidal effect.

The drug is active against microorganisms producing β-lactamases and fast-growing atypical mycobacteria.

The following are sensitive to the drug: Staphylococcus aureus, Staphylococcus epidermidis, Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Citrobacter spp., Klebsiella spp. (including Klebsiella pneumonia), Enterobacter spp., Hafnia spp., Proteus spp. (including Proteus mirabilis, Proteus vulgaris – indole-positive and indole-negative), Salmonella spp., Shigella spp. (including Shigella sonnei), Yersinia enterocolitica, Campylobacter jejuni, Aeromonas hydrophila, Plesiomonas aeruginosa, Vibrio cholerae, Vibrio parahaemolyticus, Haemophilus influenzae, Chlamydia spp., Legionella spp., Serratia spp., Providencia spp., Haemophilus ducreyi, Bordetella parapertussis, Bordetella pertussis, Moraxella catarrhalis, Propionibacterium acne, Brucella spp.

The following have varying sensitivity to the drug: Enterococcus faecalis, Streptococcus pyogenes, Streptococcus pneumoniae, Streptococcus viridans, Serratia marcescens, Pseudomonas aeruginosa, Acinetobacter spp., Mycoplasma hominis, Mycoplasma pneumoniae, Mycobacterium tuberculosis, Mycobacterium fortuitum, Ureaplasma urealyticum, Clostridium perfringens, Corynebacterium spp., Helicobacter pylori, Listeria monocytogenes, Gardnerella vaginalis.

In most cases, the following are not sensitive to the drug: Nocardia asteroides, anaerobic bacteria (for example, Bacteroides spp., Peptococcus spp., Peptostreptococcus spp., Eubacterium spp., Fusobacterium spp., Clostridium difficile).

Ofloxacin does not act on Treponema pallidum.

Pharmacokinetics

After a single 60-minute IV infusion of 200 mg of ofloxacin, the average C_max is 2.7 µg/ml; 12 hours after administration, the concentration is 0.3 µg/ml. C_ss is achieved after administration of 4 doses.

The average C_ss^max and C_ss^min are achieved after IV administration of 200 mg of ofloxacin every 12 hours for 7 days and are 2.9 and 0.5 µg/ml, respectively.

Ofloxacin widely penetrates into many body fluids and tissues, including saliva, bronchial secretions, bile, tear and cerebrospinal fluid, pus, lungs, prostate gland, and skin.

Ofloxacin undergoes partial (5%) metabolism in the liver. Plasma protein binding is 20-25%.

The T_1/2 of ofloxacin is 6-7 hours. Up to 80% of the orally administered drug is excreted by the kidneys unchanged, a small part of the active substance is also excreted in the feces. During hemodialysis, 10-30% of the drug is removed.

In patients with impaired renal function (creatinine clearance ≤50 ml), the T_1/2 of ofloxacin increases.

Indications

• Respiratory tract infections (bronchitis, pneumonia);
• ENT organ infections (sinusitis, pharyngitis, otitis media, laryngitis);
• Skin and soft tissue infections;
• Bone and joint infections;
• Infectious and inflammatory diseases of the abdominal cavity and biliary tract (except for bacterial enteritis);
• Kidney infections (pyelonephritis), urinary tract infections (cystitis, urethritis);
• Pelvic organ infections (endometritis, salpingitis, oophoritis, cervicitis, parametritis, prostatitis);
• Genital organ infections (colpitis, orchitis, epididymitis);
• Gonorrhea;
• Chlamydia;
• Septicemia;
• Meningitis;
• Prevention of infections in patients with impaired immune status (including neutropenia).

ICD codes

Dosage Regimen

Tablets

Orally. Doses are selected individually depending on the location, severity of the infection, sensitivity of microorganisms, as well as the general condition of the patient and the function of the liver and kidneys.

For adults – 200-800 mg/day, frequency of administration – 2 times/day, course of treatment – 7-10 days. A dose of up to 400 mg/day can be prescribed in a single dose, preferably in the morning.

For gonorrhea – 400 mg as a single dose.

In patients with impaired renal function (with CC 50-20 ml/min), a single dose should be 50% of the average dose with a frequency of administration of 2 times/day, or the full single dose is administered once/day. With CC less than 20 ml/min, a single dose is 200 mg, then – 100 mg/day every other day.

For hemodialysis and peritoneal dialysis, the drug is prescribed at 100 mg every 24 hours.

The maximum daily dose for hepatic insufficiency is 400 mg/day.

The tablets should be taken whole, with water, before or during meals.

The duration of treatment is determined by the sensitivity of the pathogen and the clinical picture; treatment should be continued for at least another 3 days after the disappearance of disease symptoms and complete normalization of temperature. In the treatment of salmonellosis, the course of treatment is 7-8 days, for uncomplicated lower urinary tract infections, the course of treatment is 3-5 days.

Solution

IV drip. Doses are selected individually depending on the location and severity of the infection, as well as the sensitivity of microorganisms, the general condition of the patient and the function of the liver and kidneys.

IV drip infusion begins with a single dose of 200 mg, which is administered slowly over 30-60 minutes. When the patient’s condition improves, they are switched to oral administration of the drug at the same daily dose.

Urinary tract infections – 100 mg 1-2 times/day, kidney and genital organ infections – from 100 mg 2 times/day to 200 mg 2 times/day, respiratory tract infections, as well as ENT organ infections, skin and soft tissue infections, bone and joint infections, abdominal infections, septic infections – 200 mg 2 times/day. If necessary, the dose can be increased to 400 mg 2 times/day.

For prevention of infections in patients with severe immunodeficiency – 400-600 mg/day.

If necessary, IV drip – 200 mg in a 5% glucose solution. The duration of infusions is 30 minutes. Only freshly prepared solutions should be used.

In patients with impaired renal function (with creatinine clearance (CC) 50-20 ml/min), a single dose should be 50% of the average dose with a frequency of administration of 2 times/day, or the full single dose is administered once/day. With CC less than 20 ml/min, a single dose is 200 mg, then – 100 mg/day every other day.

For hemodialysis and peritoneal dialysis – 100 mg every 24 hours.

The maximum daily dose for hepatic insufficiency is 400 mg/day.

Adverse Reactions

From the CNS: headache, seizures, numbness and paresthesia of the extremities, dizziness, depression, intense dreams, nightmares, psychomotor agitation, unsteadiness of movements, tremor; psychotic reactions, anxiety, phobias, confusion, hallucinations, increased intracranial pressure.

From the senses: impaired color perception, diplopia, disturbances of taste, smell, hearing and balance.

From the digestive system: gastralgia, anorexia, nausea, vomiting, diarrhea, flatulence, abdominal pain, increased activity of hepatic transaminases, hyperbilirubinemia, cholestatic jaundice, pseudomembranous enterocolitis.

From the musculoskeletal system: tendinitis, myalgia, arthralgia, tenosynovitis, tendon rupture;

From the cardiovascular system: tachycardia, decreased blood pressure (with IV administration; if blood pressure drops sharply, administration is stopped), vasculitis, collapse.

From the urinary system: acute interstitial nephritis, impaired renal function, hypercreatininemia, increased urea content.

From the hematopoietic organs: leukopenia, agranulocytosis, anemia, thrombocytopenia, pancytopenia, hemolytic and aplastic anemia.

From the skin: petechiae, bullous hemorrhagic dermatitis, papular rash with crusts, indicating vascular damage (vasculitis).

Allergic reactions: skin rash, skin itching, urticaria, allergic pneumonitis, allergic nephritis, eosinophilia, fever, angioedema, bronchospasm; multiforme exudative erythema (including Stevens-Johnson syndrome) and toxic epidermal necrolysis (Lyell’s syndrome), photosensitivity, anaphylactic shock.

Other: dysbacteriosis, superinfection, vaginitis, hypoglycemia (in patients with diabetes mellitus).

Local reactions: pain, redness at the injection site, thrombophlebitis (with IV administration).

Contraindications

• Glucose-6-phosphate dehydrogenase deficiency;
• Epilepsy (including history);
• CNS lesions with a lowered seizure threshold (after traumatic brain injury, stroke, inflammatory brain diseases);
• Pregnancy;
• Lactation;
• Childhood and adolescence (up to 18 years), until skeletal growth is complete;
• Hypersensitivity or intolerance to ofloxacin and other fluoroquinolone derivatives.

Caution should be exercised when prescribing the drug to patients with cerebral atherosclerosis, cerebrovascular accident (in history), organic CNS lesions, chronic renal failure.

Use in Pregnancy and Lactation

Contraindicated during pregnancy and lactation.

Use in Hepatic Impairment

The maximum daily dose for hepatic insufficiency is 400 mg/day.

Use in Renal Impairment

In patients with impaired renal function (with creatinine clearance (CC) 50-20 ml/min), a single dose should be 50% of the average dose with a frequency of administration of 2 times/day, or the full single dose is administered once/day. With CC less than 20 ml/min, a single dose is 200 mg, then – 100 mg/day every other day.

For hemodialysis and peritoneal dialysis – 100 mg every 24 hours.

Pediatric Use

In children, it is used only in life-threatening situations, taking into account the expected benefit and the potential risk of side effects, when it is impossible to use other, less toxic drugs. The average daily dose in this case is 7.5 mg/kg, the maximum is 15 mg/kg.

Special Precautions

It is not the drug of choice for pneumonia caused by pneumococci. It is not indicated for the treatment of acute tonsillitis.

It is not recommended to use for more than 2 months, to be exposed to sunlight, or to UV radiation (mercury-quartz lamps, solarium).

In case of side effects from the CNS, allergic reactions, pseudomembranous colitis, discontinuation of the drug is necessary. For pseudomembranous colitis, confirmed by colonoscopy and/or histologically, oral administration of vancomycin and metronidazole is indicated.

Rarely occurring tendinitis can lead to tendon rupture (primarily the Achilles tendon), especially in elderly patients. If signs of tendinitis appear, it is necessary to immediately stop treatment, immobilize the Achilles tendon and consult an orthopedist.

During treatment, ethanol should not be consumed.

When using the drug, women are not recommended to use hygienic tampons due to an increased risk of developing candidiasis.

During treatment, worsening of myasthenia gravis and increased frequency of porphyria attacks in predisposed patients may occur.

It may lead to false-negative results in the bacteriological diagnosis of tuberculosis (it inhibits the isolation of *Mycobacterium tuberculosis*).

In patients with impaired liver or kidney function, monitoring of the plasma concentration of ofloxacin is necessary. In severe renal and hepatic insufficiency, the risk of toxic effects increases (dose adjustment is required).

In children, it is used only in life-threatening situations, taking into account the expected benefit and the potential risk of side effects, when it is impossible to use other, less toxic drugs. The average daily dose in this case is 7.5 mg/kg, and the maximum dose is 15 mg/kg.

Effect on the Ability to Drive Vehicles and Mechanisms

During treatment, it is necessary to refrain from driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

Symptoms: dizziness, confusion, lethargy, disorientation, drowsiness, vomiting.

Treatment: gastric lavage, symptomatic therapy.

Drug Interactions

It is compatible with the following infusion solutions: isotonic sodium chloride solution, Ringer’s solution, 5% fructose solution, 5% dextrose solution. Do not mix with heparin (risk of precipitation).

It reduces the clearance of theophylline by 25% (when used concomitantly, the dose of theophylline should be reduced).

Cimetidine, furosemide, methotrexate, and drugs that block tubular secretion increase the plasma concentration of ofloxacin.

It increases the plasma concentration of glibenclamide.

When taken concomitantly with vitamin K antagonists, monitoring of the blood coagulation system is necessary.

When prescribed with NSAIDs, nitroimidazole derivatives, and methylxanthines, the risk of neurotoxic effects increases.

When prescribed concomitantly with corticosteroids, the risk of tendon rupture increases, especially in the elderly.

When prescribed with drugs that alkalinize urine ( carbonic anhydrase inhibitors, citrates, sodium bicarbonate), the risk of crystalluria and nephrotoxic effects increases.

Storage Conditions

Store at a temperature not exceeding 25°C (77°F) in a place protected from light. Do not freeze. Keep out of the reach of children.

Shelf Life

The shelf life is 3 years. Do not use after the expiration date printed on the package.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.